Recent advances in drug delivery and formulation最新文献

Background: Curcumin has been shown to possess anti-inflammatory and antimicrobial properties, offering potential benefits in burn management. Coconut oil has also been reported to possess skin-moisturizing, antimicrobial, and anti-inflammatory properties. This study aimed to develop and evaluate curcumin-loaded coconut oil-based emulgel formulations to improve therapeutic outcomes in burn management.

Methods: Eight emulgel formulations (F1-F8) were prepared using lecithin, hyaluronic acid, and coconut oil. The formulations were assessed for organoleptic properties (color, smell, texture, phase separation) and physicochemical characteristics, including pH (5.40-6.35), viscosity (3840-5369 cps), spreadability (7-8 cm), drug content (82-95%), and in vitro drug release (88-93%). Light microscopy and scanning electron microscopy (SEM) were used to analyze the structural characteristics. Drug release kinetics were evaluated using the Hixson-Crowell model.

Results: The formulations exhibited a bi-continuous system with a three-dimensional network structure. The developed formulations were evaluated for pH (5.40-6.35), viscosity (3840-5369 cps), spreadability (7-8 cm), drug content (82-95%), and in vitro drug release (88-93%) over 24 hours which showed promising result for topical delivery. Among the formulations, F3 demonstrated the highest drug release, whereas F8 exhibited the highest viscosity and drug content. The emulgel also provided cooling, moisturizing, anti-inflammatory, and antimicrobial effects, supporting wound healing and pain relief.

Conclusion: The developed Curcumin-loaded coconut oil-based emulgel shows promise for burn management, offering enhanced topical drug delivery and therapeutic benefits. These findings support further research to optimize formulation parameters for improved clinical outcomes.

A potential class of cutting-edge medication delivery devices, nanosponges have become an effective tool for managing drug overdoses and detoxification. The capacity to adsorb and sequester a variety of toxins, such as heavy metals, bacterial endotoxins, and medications, makes these highly porous, biocompatible, and biodegradable particles-which are usually made from crosslinked polymers-an effective way to remove toxins. Nanosponges' adaptability enables their use in a number of sectors, including drug-resistant illness treatment, environmental remediation, and acute poisoning treatment. Detoxification and targeted drug release for diseases like cancer, heart disease, and neurological problems are made possible by the controlled delivery of therapeutic substances using nanosponges. With a focus on their capacity to improve medication bioavailability and lower systemic toxicity, this study examines the mechanism of action, design approaches, and therapeutic potential of nanosponges in detoxification. The paper also discusses new developments in the sector, such as how they can be used to treat drug overdoses and how nanosponges can help stop and lessen the negative effects of environmental contaminants. Despite its potential, there are still obstacles to overcome in order to maximize nanosponges' manufacturing, scalability, and regulatory acceptance. In order to optimize their potential in therapeutic treatments, this review attempts to give a thorough overview of the most recent advancements in detoxifying nanosponges, their clinical uses, and future research objectives.

Background: Dysphagia is a challenging medical condition that significantly affects individuals' swallowing function, quality of life, and overall well-being, especially in geriatric and pediatric populations. Sprinkle formulations are emerging as a broadly accepted solution to this challenge. However, such formulations are quite challenging to formulate as modified-release delivery systems. The present study aims to resolve this issue by formulating modified-release minitabs of the model drug etoricoxib as a sprinkle formulation.

Methods: A fabricated metal mold and punch system was used to manually manufacture minitabs with a diameter of 3.2 mm and a weight of approximately 22 mg. The formulation derived from trial batches was further optimized using a 3 × 2 complete factorial design, as implemented in Stat- Ease Design Expert 7.0 software (trial version). Independent factors HPMC K4M (X1) and K100M (X2) were optimized against dependent factors: Hardness (R1), Friability (R2), and Drug release at 2 hrs (R3), 4 hrs (R4), and 8 hrs (R5).

Result: The derived, optimized formulation, based on a desirability function, sustained drug release for up to 8 hours and met all the acceptance criteria. The final dosage form was designed as a hard gelatin capsule filled with approximately 22 minitabs, in the form of a sprinkle formulation, to be sprinkled over soft foods for administration.

Conclusion: As the formulation was designed using a model drug, further investigations with other drugs can also be done with relevant changes in the optimized formulation. In summary, it can also be utilized as a platform for developing modified-release sprinkle formulations of other drugs.

Introduction: The purpose of this study was to develop sustained-release enteric-coated granules of Amla extract and Esomeprazole Magnesium for the treatment of peptic ulcer. It is well known that Amla possesses anti-ulcer activity due to the phenolic compound gallic acid, which inhibits a gastric H+/K+ ATPase pump. Therefore, enteric-coated Amla extract granules were combined with Esomeprazole Magnesium granules to enhance the synergistic effect, mitigate adverse effects associated with esomeprazole magnesium and improve overall anti-ulcer activity, while the enteric-coated multiparticulate system ensures prolonged drug release with a minimum dose.

Methods: A Soxhlet extraction method was employed to obtain the Amla phenolic extract, using a solvent mixture of ethanol and water in a 7:3 ratio. Wet granulation techniques were utilized to prepare granules, and hydroxypropyl methylcellulose phthalate served as the enteric coating agent. The in vitro drug release and drug entrapment were used to optimize the enteric-coated granules of Amla extract and Esomeprazole Magnesium. An in vivo study was conducted in Wistar albino rats (120-140 g) of both sexes to demonstrate the antiulcer activity of the developed formulation against an aspirin-induced ulcerated rat model.

Results: Both in vitro and in vivo studies were conducted. In the in vitro studies, drug release was assessed at pH 1.2 (simulated gastric fluid) and pH 6.8 (simulated intestinal fluid). The results demonstrated negligible drug release in the simulated gastric fluid due to the protective enteric coating, while efficient drug release occurred in the simulated intestinal fluid. In the in vivo studies, the combination therapy showed a significant therapeutic effect compared to other treatment groups in an animal model.

Discussion: Amla extract and Esomeprazole Magnesium were combined to prepare sustainedrelease enteric-coated granules for the treatment of peptic ulcers. The phenolic substance gallic acid inhibits the gastric H+/K+ ATPase pump, hence enhancing anti-ulcer efficacy. The combination demonstrated substantial therapeutic efficacy in both in vitro and in vivo investigations.

Conclusion: The amla extract and esomeprazole magnesium enteric-coated granules with sustained release and negligible drug release in acidic pH were achieved. In the in vivo studies, the combination therapy demonstrated a significant positive effect in treating peptic ulcers in a rat ulcer model, as shown by assessments of various parameters such as ulcer index, total gastric juice acidity, hematological analysis, and histopathological evaluations.

Introduction: Onychomycosis is a frequently occurring fungal infection that affects the nails of the fingers and toes. Infection is caused by yeasts, dermatophytes, and nondermatophyte molds. Onychomycosis should be confirmed by mycology. Diagnosis can be made by various techniques, such as microscopy, fungal culture, potassium hydroxide, polymerase chain reaction, and histopathology. This review was undertaken to study the challenges associated with topical therapy of onychomycosis and techniques to overcome these challenges.

Methods: The search engines used for carrying out the literature review were PubMed, Google, Scopus, and Google Scholar. The search terms employed were "topical therapies for onychomycosis", "diagnosis of onychomycosis", and "challenges in the treatment of onychomycosis". The data related to topical treatments were compiled, and articles available in English language were only considered.

Results and discussion: The main challenge associated with topical therapy was found to be the unique structure of the nails, hampering drug penetration to the infection site and inducing fungal drug resistance. Conventional treatment methods, as well as novel techniques developed for topical therapy, like microporation, ionotophoresis, laser, and photodynamic therapy, have also been explored. Oral antifungals are most commonly used for moderate to severe onychomycosis as they provide greater cure rates, whereas topical application of antifungals is advocated for mild to moderate infections as it possesses a better safety profile. Efinaconazole solution (10%), tavaborole solution (5%), and ciclopirox nail lacquer (8%) for topical use are accepted by the Food and Drug Administration (FDA) for the management of onychomycosis. Laser treatment is approved in the United States for the short-term improvement of clear nails in fungal infections, but the clinical outcomes have not yet reached optimal levels.

The treatment of neurodegenerative illnesses remains a substantial problem due to the blood-brain barrier's restrictive nature, which restricts therapeutic agent penetration. Phospholipid Nanocomplexes (PNCs) have emerged as next-generation neurotherapeutics, utilizing natural BBB transport pathways to improve drug delivery. These nanocarriers, with lipid-based architectures, allow for receptor-mediated transcytosis, lipid raft-mediated transport, and adsorptive-mediated endocytosis, resulting in precise and sustained drug release inside the central nervous system. Recent preclinical and clinical studies have shown that PNC-based formulations of neurotrophic factors, antioxidants, and gene-silencing therapies significantly improve neuronal survival, cognitive function, and neuroprotection in conditions like Alzheimer's Disease (AD), Parkinson's Disease (PD), Glioblastoma (GBM), and multiple sclerosis. Despite the positive outcomes, issues such as scalability, long-term safety, and regulatory approval remain. This study critically assesses the present status of PNC-based neurotherapeutics, emphasizing their benefits over traditional therapies, analyzing the most recent clinical trial outcomes, and assessing difficulties and future prospects. To improve PNC effectiveness, the potential for artificial intelligence-driven medication design, multifunctionalized nanocarriers, and hybrid biomaterial methods is investigated. As biocompatible and patientspecific nanomedicine advances, PNCs represent a breakthrough approach to precision neuroscience, providing tailored, efficient, and safer therapies for neurodegenerative diseases.

Pharmaceutical excipients play a critical role in drug formulation, ensuring stability, bioavailability, manufacturability, and patient safety. While India has made progress in aligning with international excipient regulations, significant regulatory gaps persist, including inconsistent enforcement, lack of mandatory GMP compliance, and inadequate impurity testing standards. These challenges create quality inconsistencies and potential safety risks, particularly for high-risk excipients. Indian excipient manufacturers face difficulties meeting international regulatory expectations, such as FDA, EMA, and PMDA requirements, due to differences in documentation, quality control, and risk assessment standards. Case studies highlight successful compliance strategies, including supplier qualification, in-house impurity testing, and risk-based categorization. To strengthen excipient regulation, mandatory GMP certification, a risk-based excipient categorization system, and alignment with IPEC-PQG, WHO, and ICH Q7 guidelines are recommended. Additionally, CDSCO must enhance oversight through advanced impurity testing and improved traceability requirements. Ensuring regulatory harmonization with global standards will enhance India's competitiveness in the excipient supply chain, facilitate international market access, and improve overall drug safety and efficacy. This review underscores the urgent need for structured regulatory reforms to streamline compliance, ensure excipient quality, and strengthen India's position in the global pharmaceutical industry.

The cosmetics business is a valuable and stable multibillion-dollar business that keeps growing yearly with new, specialized goods. Natural goods contain a wealth of medicinally active chemicals used to treat a wide range of skin problems, including infections, inflammation, and damage caused by UV light and pollution. Cosmeceuticals are a mix of cosmetic and medical chemicals. Based on their main ingredients, they can be used for both beauty and health purposes. Many people think that natural goods are a great way to obtain cosmeceuticals. It has strong antiinflammatory, antibacterial, anti-cancer, and protective properties. The benefit for the skin has been said to be the most interesting. GA and its products have been used a lot as an adjuvant in many therapeutic formulations, as an alternative to hydro-cortisone in children with atopic dermatitis and other skin diseases, and as an ingredient in cosmetics because they are good for humans. GA is GRAS (generally recognized as safe) by the US Food and Drug Administration. Oxidative stress, which happens when too many free radicals build up, is the main cause of many skin diseases that get worse over time, like aging. Polyphenols, including gallic acid, represent a significant category of naturally occurring antioxidants. They have emerged as potent antioxidants suitable for incorporation into active makeup products. Recent advancements include patent filings related to novel applications and formulations of Gallic acid in cosmetic science that highlight innovative delivery systems, such as nano-formulations enhancing stability and efficacy, as well as its synergistic combinations with other active ingredients to address targeted skin concerns like pigmentation, aging, and sensitivity which meets the demands of modern consumers.

ADHD is a common condition that affects many kids in the United States, about 2 to 18 percent of children between 6 and 17 years old. ADHD manifests as hyperactivity, impulsivity, and inattention, impacting various aspects of life. Effective management involves a combination of psychostimulant medication, such as methylphenidate, and behavioral therapy. Modified-release formulations, including chewable tablets, transdermal patches, and osmotic-controlled release tablets, offer improved treatment adherence and overall quality of life. Understanding the pathophysiology involves neuroimaging studies that reveal alterations in brain regions rich in dopamine receptors. Methylphenidate, a common ADHD medication, works by inhibiting dopamine reuptake, thereby increasing extracellular dopamine levels. Different drug delivery systems, such as extended-release chewable tablets, transdermal patches, and OROS formulations, provide diverse options for individual needs. The advent of innovative formulations like methylphenidate hydrochloride extendedrelease oral suspension (Quillivant ER) and methylphenidate hydrochloride multilayer extendedrelease capsules (Aptensio XR) addresses challenges in pediatric medication administration. Recent additions like the orally disintegrating tablet (Cotempla X-ODT) offer convenience and flexibility. Understanding the pharmacokinetics, pharmacodynamics, and benefits of these formulations enhances the ability to tailor ADHD treatment to individual patient needs.

Phytoconstituents, derived from plants, possess significant therapeutic potential but often face challenges such as poor solubility and low bioavailability, limiting their efficacy. Solid dispersion (SD) is a promising approach to improve the solubility and bioavailability of these poorly water- soluble phytoconstituents. By dispersing the active drug in a hydrophilic carrier, solid dispersion enhances the surface area of the drug, improving its dissolution rate and enhancing absorption. This review provides an overview of the various generations of solid dispersions, highlighting the evolution from crystalline carriers in first-generation solid dispersions to the more advanced amorphous solid solutions in second and third-generation formulations, which offer enhanced solubility and bioavailability. The article also discusses various techniques for preparing solid dispersions, including solvent evaporation, melting, and spray-drying methods, and emphasizes the importance of selecting appropriate carriers, such as hydrophilic polymers, to optimize the dissolution rate of phytoconstituents. The study highlighted the recent case studies on several phytochemicals, like alkaloids, glycosides, Polyphenols, etc., demonstrating the effectiveness of solid dispersion in improving their solubility and therapeutic performance. Additionally, the review addresses the challenges related to the solubility of phytoconstituents and their impact on drug absorption, as well as the role of solid dispersion in overcoming these challenges. Overall, solid dispersion technology emerges as a versatile and effective tool for enhancing the oral bioavailability of phytoconstituents, paving the way for more efficient herbal therapies in modern medicine.